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1. 发明申请

US20110105535A1 INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE 有权
标题翻译：磷脂酰肌醇3激酶抑制剂
公开(公告)号：US20110105535A1
公开(公告)日：2011-05-05
申请号：US13005132
申请日：2011-01-12
申请人： Ian BRUCE , Bernard Cuenoud , Thomas Hugo Keller , Gaynor Elizabeth Pilgrim , Nicola Press , Darren Mark Le Grand , Cathy Ritchie , Barbara Valade , Judy Hayler , Emma Budd
发明人： Ian BRUCE , Bernard Cuenoud , Thomas Hugo Keller , Gaynor Elizabeth Pilgrim , Nicola Press , Darren Mark Le Grand , Cathy Ritchie , Barbara Valade , Judy Hayler , Emma Budd
IPC分类号： A61K31/506 , C07D417/14 , A61P3/04 , C07D471/04 , A61P11/00 , A61P37/08 , A61P35/00 , A61P1/00 , A61P3/10
CPC分类号： A61K31/5377 , A61K31/497 , A61K45/06 , C07D417/04 , C07D417/14
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase.Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式的式I化合物，其中R 1，R 2，R 3和R 4具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

2. 发明授权

US08404684B2 Inhibitors of phosphatidylinositol 3-kinase 有权
标题翻译：磷脂酰肌醇3-激酶抑制剂
公开(公告)号：US08404684B2
公开(公告)日：2013-03-26
申请号：US13005132
申请日：2011-01-12
申请人： Ian Bruce , Bernard Cuenoud , Thomas Hugo Keller , Gaynor Elizabeth Pilgrim , Nicola Press , Darren Mark Le Grand , Cathy Ritchie , Barbara Valade , Judy Hayler , Emma Budd
发明人： Ian Bruce , Bernard Cuenoud , Thomas Hugo Keller , Gaynor Elizabeth Pilgrim , Nicola Press , Darren Mark Le Grand , Cathy Ritchie , Barbara Valade , Judy Hayler , Emma Budd
IPC分类号： C07D417/04 , A61K31/506
CPC分类号： A61K31/5377 , A61K31/497 , A61K45/06 , C07D417/04 , C07D417/14
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式的式I化合物，其中R 1，R 2，R 3和R 4具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

3. 发明授权

US06589950B1 Purine derivatives inhibitors of tyrosine protein kinase SYK 有权
标题翻译：嘌呤衍生物酪氨酸蛋白激酶SYK抑制剂
公开(公告)号：US06589950B1
公开(公告)日：2003-07-08
申请号：US10048577
申请日：2002-03-19
申请人： Stephen Paul Collingwood , Judy Hayler , Darren Mark Le Grand , Henri Mattes , Keith Allan Menear , Clive Victor Walker , Xiao-Ling Cockcroft
发明人： Stephen Paul Collingwood , Judy Hayler , Darren Mark Le Grand , Henri Mattes , Keith Allan Menear , Clive Victor Walker , Xiao-Ling Cockcroft
IPC分类号： C07D47316
CPC分类号： C07D473/24 , A61K31/52 , C07D473/16 , C07D473/18
摘要： Disclosed are compounds of the formula in free or salt form, wherein X, R1, R2, R3, and R4 are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
摘要翻译：公开的是无游离或盐形式的化合物，其中X，R 1，R 2，R 3和R 4如本说明书中所定义，其制备及其作为药物的用途，特别是用于治疗炎性或阻塞性气道疾病。

4. 发明申请

US20080280871A1 5-Phenyl-4-Methyl-Thiazol-2-Yl-Amine Derivatives as Inhibitors of Phosphatidylin Ositol 3 Kinase Enzymes (PI13) For Treatment of Inflammatory Diseases 失效
标题翻译： 5-苯基-4-甲基 - 噻唑-2-基胺衍生物作为磷脂酰肌醇蛋白的抑制剂Ositol 3激酶（PI13）用于治疗炎性疾病
公开(公告)号：US20080280871A1
公开(公告)日：2008-11-13
申请号：US10568053
申请日：2004-08-27
申请人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine Leblanc , Darren Mark Le Grand , Clive McCarthy
发明人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine Leblanc , Darren Mark Le Grand , Clive McCarthy
IPC分类号： A61K31/426 , C07D277/42 , C07D417/12 , A61K31/5377 , A61P17/06 , A61P11/00
CPC分类号： C07D451/04 , C07D277/48 , C07D417/12 , C07D471/04
摘要： in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式，其中R a，R b，R b，R 3，R 3，R SUP > 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

5. 发明申请

US20110124693A1 5-PHENYL-4-METHYL-THIAZOL-2-YL-AMINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3 KINASE ENZYMES (PI3) FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： 5-苯基-4-甲基 - 噻唑-2-基胺衍生物作为磷酸胆碱酯酶3激酶（PI3）的抑制剂治疗炎症性疾病
公开(公告)号：US20110124693A1
公开(公告)日：2011-05-26
申请号：US13020211
申请日：2011-02-03
申请人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine Leblanc , Darren Mark Le Grand , Clive McCarthy
发明人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine Leblanc , Darren Mark Le Grand , Clive McCarthy
IPC分类号： A61K31/427 , A61P11/00 , A61P35/00 , A61P11/06 , A61P29/00 , A61P9/10 , A61P3/10 , A61P3/04 , A61P9/00 , A61P37/08 , A61P17/06
CPC分类号： C07D451/04 , C07D277/48 , C07D417/12 , C07D471/04
摘要： Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：式I化合物：游离或盐形式，其中R a，R b，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

6. 发明申请

US20110124624A1 5-PHENYL-4-METHYL-THIAZOL-2-YL-AMINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3 KINASE ENZYMES (PI3) FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： 5-苯基-4-甲基 - 噻唑-2-基胺衍生物作为磷酸胆碱酯酶3激酶（PI3）的抑制剂治疗炎症性疾病
公开(公告)号：US20110124624A1
公开(公告)日：2011-05-26
申请号：US13020247
申请日：2011-02-03
申请人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine LeBlanc , Darren Mark Le Grand , Clive McCarthy
发明人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine LeBlanc , Darren Mark Le Grand , Clive McCarthy
IPC分类号： A61K31/426 , C07D417/12 , A61K31/4439 , C07D277/48 , A61K31/427 , A61K31/5377 , C07D451/04 , A61K31/46 , A61K31/496 , C07D471/04 , A61K31/437 , A61K31/4245 , A61K31/433 , A61P17/06 , A61P35/00 , A61P3/04 , A61P3/10 , A61P9/10 , A61P29/00 , A61P37/06
CPC分类号： C07D451/04 , C07D277/48 , C07D417/12 , C07D471/04
摘要： Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：式I化合物：游离或盐形式，其中R a，R b，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

7. 发明授权

US07902375B2 5-phenyl-4-methyl-thiazol-2-yl-amine derivatives as inhibitors of phosphatidylin ositol 3 kinase enzymes (PI13) for treatment of inflammatory diseases 失效
标题翻译： 5-苯基-4-甲基 - 噻唑-2-基 - 胺衍生物作为用于治疗炎症性疾病的磷脂酰骨甙硫蛋白3激酶（PI13）的抑制剂
公开(公告)号：US07902375B2
公开(公告)日：2011-03-08
申请号：US10568053
申请日：2004-08-27
申请人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine Leblanc , Darren Mark Le Grand , Clive McCarthy
发明人： Graham Charles Bloomfield , Ian Bruce , Judy Fox Hayler , Catherine Leblanc , Darren Mark Le Grand , Clive McCarthy
IPC分类号： A61K31/427 , C07D417/12
CPC分类号： C07D451/04 , C07D277/48 , C07D417/12 , C07D471/04
摘要： in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：其中R a，R b，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

8. 发明授权

US06670379B2 Piperidine compounds for use as ccr-3 inhibitors 失效
标题翻译：用作ccr-3抑制剂的哌啶化合物
公开(公告)号：US06670379B2
公开(公告)日：2003-12-30
申请号：US10332642
申请日：2003-04-17
申请人： Trevor John Howe , Gurdip Bhalay , Darren Mark Le Grand , Thomas Storz
发明人： Trevor John Howe , Gurdip Bhalay , Darren Mark Le Grand , Thomas Storz
IPC分类号： A61F31445
CPC分类号： C07D401/06 , C07D211/32 , C07D405/06 , C07D417/06
摘要： Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3, or 4, with the proviso that when Ar1 is p-chlorophenyl and R1 is hydrogen, R2 is not phenyl or p-nitrophenyl. The compounds are useful as pharmaceuticals.
摘要翻译：游离或盐形式的式（I）化合物，其中Ar 1是被一个或多个卤素原子取代的苯基，Ar 2是未取代的或被一个或多个选自卤素，氰基的取代基取代的苯基或萘基，羟基，硝基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基或C 1 -C 8 - 烷氧基羰基，R 1是氢或任选被羟基取代的C 1 -C 8烷基，烷氧基，酰氧基，N（R 2）R 3，卤素，羧基，C 1 -C 8 - 烷氧基羰基，-CON（R 4）R 5或一价环状有机基团R 2 和R 3各自独立地为氢或C 1 -C 8烷基，或R 2为氢，R 3为酰基或-SO 2 R 6，或R 2和R 3与它们所连接的氮原子表示5或6元杂环基团，R 4和R 5各自独立地为氢或C 1 -C 8 - 烷基，或R 4和R 5与它们所连接的氮原子表示5或6元杂环基，R 6是C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基或任选取代的苯基由C 1 -C 8烷基构成，n为1,2,3或4，条件是当Ar 1为对氯苯基且R 1为氢时，R 2不为苯基或p - 硝基苯基。这些化合物可用作药物。

9. 发明授权

US09630945B2 Autotaxin inhibitors 有权
公开(公告)号：US09630945B2
公开(公告)日：2017-04-25
申请号：US14653649
申请日：2013-12-17
申请人： Vikki Furminger , Owen Rhys Hughes , Darren Mark Le Grand , Emily Stanley , Christopher Thomson
发明人： Vikki Furminger , Owen Rhys Hughes , Darren Mark Le Grand , Emily Stanley , Christopher Thomson
IPC分类号： C07D401/12 , A61K31/454 , C07D451/04 , A61K31/4192 , A61K31/445 , A61K31/46 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D211/32 , C07D211/60 , C07D249/04 , C07D265/30 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D401/06 , C07D263/38 , C07D211/26 , C07D211/34 , C07D211/58
CPC分类号： C07D401/12 , A61K31/4192 , A61K31/445 , A61K31/454 , A61K31/46 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D211/26 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D249/04 , C07D263/38 , C07D265/30 , C07D401/06 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D451/04
摘要： The present invention relates to novel compounds of formula (I) (I) that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.

10. 发明授权

US07288537B2 Azetidine derivatives as CCR-3 receptor antagonists 失效
标题翻译：氮杂环丁烷衍生物作为CCR-3受体拮抗剂
公开(公告)号：US07288537B2
公开(公告)日：2007-10-30
申请号：US10507139
申请日：2003-03-14
申请人： Darren Mark Le Grand , Clive McCarthy , Clive Victor Walker , John James Woods
发明人： Darren Mark Le Grand , Clive McCarthy , Clive Victor Walker , John James Woods
IPC分类号： A61K31/397 , C07D205/00
CPC分类号： C07D401/12 , C07D205/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein Ar, X, Y, R1, R2, R3, R5, m, n, p and q have the meanings as indicated in the specification, are useful for treating conditions mediated by CCR3. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：游离或盐形式的式I化合物，其中Ar，X，Y，R 1，R 2，R 3，R SUP m，n，p和q具有说明书中所示的含义，可用于治疗由CCR3介导的病症。还描述了含有化合物的药物组合物和用于制备化合物的方法。

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